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Atglistatin

CAS No. : 1469924-27-3

MCE 国际站：Atglistatin

产品活性：Atglistatin 是一种选择性的脂肪甘油三酯脂酶 (ATGL) 抑制剂，体外抑制脂解作用，IC₅₀ 为 0.7 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：ATGL

In Vitro: Atglistatin inhibits Triacylglycerol (TG) hydrolase activity of wild-type white adipose tissue (WAT) in a dose-dependent manner up to 78% at the highest concentration. In comparison to wild-type preparations, TG hydrolase activity in WAT lysates from ATGL-ko animals is reduced by approximately 70% and Atglistatin had only a moderate effect on the residual activity. The combined use of Atglistatin and the hormone-sensitive lipase (HSL) inhibitor Hi 76-0079 leads to an almost complete inhibition (-95%) of TG hydrolase activity of WAT which implicates that most of the non-ATGL activity can be ascribed to HSL.

In Vivo: Animals receive Atglistatin dissolved in olive oil by oral gavage. After application, blood and tissues are collected for determination of plasma parameters, tissue Triacylglycerol (TG) levels, and inhibitor concentrations. Time-course experiments revealed that the lipolytic parameters fatty acids (FA) and glycerol are reduced 4 and 8 hours after application and returned to normal after 12 hours. Eight hours after treatment, a dose-dependent decrease is observed in FA and glycerol levels up to 50% and 62%, respectively. Atglistatin also caused a strong reduction in plasma TG levels (-43%) while blood glucose, total cholesterol, ketone bodies, and insulin levels do not significantly change. Dose and time-dependent inhibition of lipolysis is also observed in response to intraperitoneal injection of Atglistatin.

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